83782-13-2Relevant academic research and scientific papers
Metal- and base-free regioselective thiolation of the methyl C(sp3)-H bond in 2-picoline: N -oxides
Wang, Dong,Liu, Zhenlin,Wang, Zhentao,Ma, Xinyue,Yu, Peng
supporting information, p. 157 - 163 (2019/01/11)
A one-pot, two-step synthesis of pyridine-2-ylmethyl thioethers is developed through a TFAA-mediated [3,3]-sigmatropic rearrangement of pyridine N-oxides and TBAB-catalyzed direct conversion of trifluoroacetates into thioethers under metal- and base-free conditions. This methodology enables thiolation of the unactivated methyl C(sp3)-H bond in 2-picolines with thiols. Remarkable features of the method include high regioselectivity, step- and atom-economy, mild conditions, simple operation, wide substrate scope and scalability. Furthermore, the method has been successfully applied to the synthesis of omeprazole sulfide and rabeprazole sulfide without the need for TBAB catalysis. A comprehensive green chemistry metrics analysis indicated that this method is much more efficient and greener than the reported synthesis of rabeprazole sulfide.
Synthesizing method of 2-pyridine methyl sulfide and synthesizing process of related drugs
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Paragraph 0036-0038; 0063-0066, (2019/01/23)
The invention relates to a simple synthesizing method of 2-pyridine methyl sulfide and related drugs. The method is characterized in that 2-methyl pyridine n-oxide is used as the raw material and pyridine n-oxide or dichloromethane is used as the solvent to have reaction with trifluoroacetic anhydride to obtain a trifluoroacetate intermediate, purification is not needed, the trifluoroacetate intermediate is allowed to have reaction with thiophenol under the catalysis of lithium bromide or tetrabutyl ammonium bromide and by using toluene or ethyl acetate as the solvent to generate the 2-pyridine methyl sulfide. The method is simple to operate, cheap in reagents, easy in reagent obtaining, mild in reaction conditions, wide in substrate applicability, good in position selectivity, high in yield and the like. In addition, the method is successfully applied to the synthesizing of omeprazole sulfide and rabeprazole sulfide, and the synthesizing method does not need catalysts.
BENZAZEPINE DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND USE
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Page 198, (2010/02/06)
The present invention provides a novel benzazepine derivative represented by formula : wherein, R1 is a 5- or 6-membered aromatic ring, R2 is lower alkyl group, etc., Y is an optionally substituted imino group, ring A and ring B are independently an optionally substituted aromatic ring, W is formula -W1-X2-W2- (W1 and W2 are independently S(O)m1 (m1 is 0, 1 or 2), etc., and X2 is an optionally substituted alkylene groupetc. ), a preparation method and use thereof.
2-pyridine Derivatives: New Antiinflammatory Agents
Haviv, Fortuna,DeNet, Robert W.,Michaels, Raymond J.,Ratajczyk, James D.,Carter, George W.,Young, Patrick R.
, p. 218 - 222 (2007/10/02)
2-pyridine derivatives (1a-e) inhibited the dermal reverse passive Arthus reaction (RPAR) in the rat.In the same model, indomethacin was inactive, and hydrocortisone was active.Compounds 1a-d also significantly reduced exudate volume and white blood cell accumulation in the pleural RPAR.This pattern of activity was similar to that of hydrocortisone and different from that of indomethacin.
